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Huperzine and its derivant or its salt implantation agent, its preparation method and application

A technology of huperzine A and an implant is applied in the directions of medical preparations containing active ingredients, drug delivery, and drug combinations, which can solve the problems of inability to take medicines on time, low bioavailability, etc. The preparation process is simple and the effect of reducing toxic and side effects

Inactive Publication Date: 2008-08-20
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Based on the consideration of the above-mentioned problems, the present invention provides an implant of huperzine A and its derivatives or its salts. After one administration, the drug can be slowly decomposed and corroded by the continuous decomposition and erosion of biodegradable polymer materials. The ground is released into the body to achieve the purpose of long-term effect, avoiding the low bioavailability of traditional dosage forms, side effects such as dizziness, nausea, anxiety, and vomiting, and at the same time solving the problem that elderly patients with dementia cannot take medicine on time, which greatly improves the patient's Medication Adherence

Method used

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  • Huperzine and its derivant or its salt implantation agent, its preparation method and application
  • Huperzine and its derivant or its salt implantation agent, its preparation method and application
  • Huperzine and its derivant or its salt implantation agent, its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0048] A long rod-shaped mold was prepared with dimethylsiloxane (PDMS), and the PDMS mold was soaked in acetone for 0.5 h to fully infiltrate the surface. Dissolve 18g of PLGA in 100ml of acetone at 30°C, pour this solution on the PDMS mold, dry at 60°C for 2 hours, and after cooling sufficiently, peel off the PDMS mold, take out the PLGA cavity, and add 150mg of Huperzine A. At both ends of the cavity, 1g of PLGA film was taken and sealed by heat and pressure to form a solid huperzine A implant. Check its tightness with conductometric method. That is, put the drug-containing implant into quantitative deionized water, and detect the change of the current value after stirring. If the current value increases to a fixed value after the implant is placed, it indicates that the device leaks medicine and is a substandard product.

Embodiment 2

[0050] Soak PDMS with acetone for 0.5h to fully infiltrate the surface and use it as a rod-shaped mold. Dissolve 10g of PLA and 15g of PLGA in a mixed solvent of 100ml of acetone and 20ml of dichloromethane at 30°C, pour this solution on the PDMS mold, dry at 60°C for 2 hours, and after fully cooling, peel off the PDMS mold and take out the PLGA cavity , Add 200mg huperzine A. At both ends of the cavity, 4g of PLGA film was hot-pressed and encapsulated to make a solid huperzine A implant. And use the conductometric method to test its tightness.

Embodiment 3

[0052] Soak PDMS with acetone for 1h to fully infiltrate and use it as a rod-shaped mold. Dissolve 20g of PLA and 10g of PLGA in a mixed solvent of 100ml chloroform and 80ml tetrahydrofuran at 30°C, pour the solution on a PDMS mold, dry at 45°C for 6 hours, and after cooling fully, peel off the PDMS mold, take out the PLGA cavity, and add 600mg Huperzine A. At both ends of the cavity, 9g of PLGA film was hot-pressed and encapsulated to make a solid huperzine A implant. And use the conductometric method to test its tightness.

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Abstract

The invention provides an implantable dosage for huperzine-a and the derivatives or the salt, which comprises essentially huperzine-a, the derivatives or the salt, and macromolecule accessories. The invention is characterized in that the solid implantable dosage of the huperzine-a and the derivatives or the salt can be conveyed into the body by way of implant surgery; or the solution or gel of the implantable dosage of the huperzine-a and the derivatives or the salt are injected into the body to form semi-solid or gel implanted object. When used to cure senile diseases such as alzheimer disease and vascular dementia, The implantable dosage has the advantages of lengthened drug treating time, reduced times for drug taking, enhanced bioavailability of the huperzine-a and the derivatives or the salt, decreased poison and side effects of the drug, and greatly enhanced drug compliance of the patients.

Description

technical field [0001] The invention relates to implants of huperzine A and its derivatives or salts thereof, their preparation method and application. Background technique [0002] Huperzine A (Huperzine A), chemical name: (5R,9R,11E)-5-amino-11-ethylene-5,6,9,10-tetrahydro-7-methyl-5,9 -Methylene cycloaryl octane-2(1H)-pyridone, which is an alkaloid obtained from the phenolic part extracted from the Chinese herbal medicine Melaleuca [Huperzia serrata(Thunb)Thev], is a high-efficiency, low-toxicity and reversible acetylcholinesterase inhibitors (AChEI). In 1993, the US FDA approved it as a cholinergic agent. Pharmacological tests have proved that huperzine A and some of its derivatives are effective for treating Alzheimer's disease, vascular dementia and other senile dementias. Huperzine A and its derivatives involved in the present invention are respectively the following structures: [0003] [0004] With the improvement of today's living standards and the increasi...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/439A61P25/28
Inventor 李亚平顾王文陈伶俐
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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